Simvastatin

What is Simvastatin?

• Simvastatin (Flolipid; Zocor) is an HMG-CoA reductase inhibitor (statin) used together with diet, weight-loss, and exercise to reduce the risk of heart attack and stroke and to decrease the chance that heart surgery will be needed in people who have heart disease or who are at risk of developing heart disease.
• It is also used to decrease the amount of fatty substances such as low-density lipoprotein (LDL) cholesterol and triglycerides in the blood and to increase the amount of high-density lipoprotein (HDL) cholesterol in the blood.
• Simvastatin is also available as a fixed combination with ezetimibe under the brand name Vytorin.

Simvastatin Structural Formulae

Simvastatin3Dan

Simvastatin M5

What are the uses of this medicine?

Simvastatin (Flolipid; Zocor) is used as an adjunctive therapy to diet to:

• Reduce the risk of total mortality by reducing coronary heart disease (CHD) deaths and reduce the risk of non-fatal myocardial infarction, stroke, and the need for revascularization procedures in patients at high risk of coronary events.
• Reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C) in patients with primary hyperlipidemia (heterozygous familial and nonfamilial) and mixed dyslipidemia.
• Reduce elevated TG in patients with hypertriglyceridemia and reduce TG and VLDL-C in patients with primary dysbetalipoproteinemia (Fredrickson type lll hyperlipidemia).
• Reduce total-C and LDL-C in adult patients with homozygous familial hypercholesterolemia.
• Reduce elevated total-C, LDL-C, and Apo B in boys and postmenarchal girls, 10 to 17 years of age with heterozygous familial hypercholesterolemia after failing an adequate trial of diet therapy.

Limitations of Use:

• Simvastatin has not been studied in Fredrickson Types I and V dyslipidemias.

How does this medicine work?

• Simvastatin (sim" va stat' in) is an orally available inhibitor of hepatic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the major rate-limiting enzyme in cholesterol synthesis.
• Like other members of its class (the “statins”), simvastatin lowers total serum cholesterol and particularly low density lipoprotein (LDL) cholesterol concentrations, thereby reducing the risk of atherosclerosis and its complications – myocardial infarction and stroke.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Especially tell your doctor if you take:

• antifungal medications such as itraconazole (Sporanox), ketoconazole (Nizoral), posaconazole (Noxafil) and voriconazole (Vfend)
• clarithromycin (Biaxin, in Prevpac)
• cobicistat-containing medications (Stribild)
• cyclosporine (Gengraf, Neoral, Sandimmune)
• danazol
• erythromycin (E.E.S., E-Mycin, Erythrocin)
• gemfibrozil (Lopid)
• HIV protease inhibitors such as atazanavir (Reyataz), darunavir (Prezista), fosamprenavir (Lexiva), indinavir (Crixivan), lopinavir (in Kaletra), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra), saquinavir (Invirase), and tipranavir (Aptivus)
• nefazodone
• telaprevir (Incivek)
• telithromycin (Ketek)
• amiodarone (Cordarone, Pacerone)
• amlodipine (Norvasc, in Caduet, in Lotrel)
• anticoagulants ('blood thinners') such as warfarin (Coumadin, Jantoven)
• colchicine (Colcrys)
• digoxin (Digitek, Lanoxicaps, Lanoxin)
• diltiazem (Cardizem, Dilacor, Tiazac)
• dronedarone (Multaq)
• other cholesterol-lowering medications such as fenofibrate (Tricor), lomitapide (Juxtapid), and niacin (nicotinic acid, Niacor, Niaspan)
• ranolazine (Ranexa)
• verapamil (Calan, Covera, Isoptin, Verelan)

Is this medicine FDA approved?

• Simvastatin was approved for use in the United States in 1991 and is still widely used with more than 40 million prescriptions being filled yearly.

How should this medicine be used?

Recommended dosage:

• Dose range is 5 to 80 mg/day.
• Recommended usual starting dose is 20 to 40 mg once a day in the evening.
• Recommended starting dose for patients at high risk of CHD is 40 mg/day.

Patients with Homozygous Familial Hypercholesterolemia:

• The recommended dosage is 40 mg/day in the evening or 80 mg/day in 3 divided doses of 20 mg and an evening dose of 40 mg.

Adolescents (10 to 17 years of age) with Heterozygous Familial Hypercholesterolemia:

• The recommended usual starting dose is 10 mg once a day in the evening.
• The recommended dosing range is 10 to 40 mg/day; the maximum recommended dose is 40 mg/day.

Administration:

• Simvastatin comes as a tablet and as a suspension to take by mouth.
• The tablets are usually taken once a day in the evening.
• The suspension is usually taken once a day in the evening on an empty stomach.
• Take simvastatin at around the same time every day.
• Shake suspension well for at least 20 seconds before each use.
• If you will be taking the simvastatin suspension, do not use a household teaspoon to measure your dose.
• Instead, use a properly marked measuring device such as a medicine spoon or oral syringe.
• Ask your doctor or pharmacist if you need help getting or using a measuring device.
• Your doctor may start you on a low dose of simvastatin and gradually increase your dose, not more than once every 4 weeks.
• Continue to take simvastatin even if you feel well.
• Do not stop taking simvastatin without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 5 mg; 10 mg; 20 mg; 40 mg; 80 mg

This medicine is available in fallowing brand namesː

• Flolipid; Zocor

What side effects can this medication cause?

The most common side effects of this medicine include:

• upper respiratory infection, headache, abdominal pain, constipation, and nausea.

Additional side effects may include:

• Edema/swelling
• Abdominal pain
• Atrial fibrillation
• Constipation
• Gastritis
• Diabetes mellitus
• Myalgia
• Headache
• Insomnia
• Vertigo
• Bronchitis
• Sinusitis
• Eczema
• Infection, urinary tract

What special precautions should I follow?

• Simvastatin, like other statins, occasionally causes myopathy manifested as muscle pain, tenderness or weakness with creatine kinase (CK) above ten times the upper limit of normal (ULN). Myopathy sometimes takes the form of rhabdomyolysis with or without acute renal failure secondary to myoglobinuria, and rare fatalities have occurred. Risks increase with higher doses and concomitant use of certain CYP3A4 inhibitors, gemfibrozil, cyclosporine, danazol, amiodarone, and verapamil. Predisposing factors include advanced age (≥65), uncontrolled hypothyroidism, and renal impairment.
• Patients should be advised to report promptly any symptoms of myopathy. Simvastatin therapy should be discontinued immediately if myopathy is diagnosed or suspected.
• Persistent elevations in hepatic transaminase can occur. Monitor liver enzymes before and during treatment. Patients titrated to the 80-mg dose should receive more frequent liver function tests than patients on lower doses.
• It is recommended that liver function tests be performed before the initiation of simvastatin, and thereafter when clinically indicated. Patients titrated to the 80-mg dose should receive an additional test prior to titration, 3 months after titration to the 80-mg dose, and periodically thereafter (e.g., semiannually) for the first year of treatment.
• Women of childbearing age should be advised to use an effective method of birth control to prevent pregnancy while using simvastatin. Discuss future pregnancy plans with your patients, and discuss when to stop taking simvastatin if they are trying to conceive. Patients should be advised that if they become pregnant they should stop taking simvastatin and call their healthcare professional.
• Women who are breastfeeding should not use simvastatin. Patients who have a lipid disorder and are breastfeeding should be advised to discuss the options with their healthcare professional.
• Ask your doctor about the safe use of alcoholic beverages while you are taking simvastatin. Alcohol can increase the risk of serious side effects.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Supportive measures should be taken in the event of an overdose.
• The dialyzability of simvastatin and its metabolites in man is not known at present.

Can this medicine be used in pregnancy?

• Pregnancy Category X.

Can this medicine be used in children?

• Safety and effectiveness of simvastatin in patients 10 to 17 years of age with heterozygous familial hypercholesterolemia have been evaluated
• Simvastatin has not been studied in patients younger than 10 years of age, nor in pre-menarchal girls.
• Doses greater than 40 mg have not been studied in this population.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• SIMVASTATIN

Inactive ingredients:

• ASCORBIC ACID
• CITRIC ACID ANHYDROUS
• HYDROXYPROPYL CELLULOSE
• HYPROMELLOSE
• ANHYDROUS LACTOSE
• MAGNESIUM STEARATE
• STARCH, CORN
• TALC
• TITANIUM DIOXIDE

Who manufactures and distributes this medicine?

Manufactured by:

• Cadila Healthcare Limited
• Ahmedabad, India

Distributed by:

• Zydus Pharmaceuticals USA Inc.
• Princeton, NJ

What should I know about storage and disposal of this medication?

• Store at 20° to 25°C (68° to 77°F).
• Dispense in a tight container.

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

• Dailymed label info on Simvastatin
• FDA Simvastatin

Simvastatin Resources
Latest articles Most recent articles Ongoing trials	Wikipedia